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Article Abstract
Miltirone is a valuable bioactive natural product isolated from the well-known Chinese herb Danshen. In this study, palladium-catalyzed C(sp) - H arylation, decarboxylation and aromatization cascade approach are reported that allows the direct introduction of various aryl groups at the A-ring benzylic methylene of various miltirone substrates (CA2 - CA31). The evaluation of the cytotoxic activity was performed against three human cancer cell lines. Among the synthesized compounds, the derivative CA7 (IC = 0.45 μM) exhibited excellent MDA-MB-231 cells inhibition activity. Derivative CA7 inhibited MDA-MB-231 cells migration, significantly suppressed the colony formation downregulated mitochondrial membrane potential and induced reactive oxygen species accumulation leads to apoptosis of MDA-MB-231 cells. CA7 with potential anticancer properties warranting further development.
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| http://dx.doi.org/10.1016/j.bioorg.2025.108488 | DOI Listing |
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